Integral membrane proteins (i.e., membrane proteins permanently associated with a cell membrane) are currently being studied for their potential as drug targets. Many membrane proteins such as ion channels and G-protein coupled receptors are involved in the function and/or regulation of excitable cells. It is well known that integral membrane proteins are potential valuable drug targets for treating human disease and disorders. Current methods of screening integral membrane proteins for binding to ligands is generally carried out in whole cells. This technique has the advantage of using the proteins in their native environment which ensures proper function of the protein. Moreover, the compounds that are screened are generally small molecules and/or peptides. While techniques for screening membranes proteins have advanced dramatically in the recent years, these techniques have failed to produce clear results in a high throughput format. There continues to be a long felt but unmet need for methods that can identify novel compounds and novel mechanisms for modulating integral membrane proteins.